{"entity":{"id":"dolasetron","kind":"drug","name":"Dolasetron","aka":["Dolasetron mesylate"],"tldr":"Dolasetron is one of the serotonin-blocking antiemetics that transformed chemotherapy in the 1990s, approved in 1997 to prevent nausea and vomiting; its intravenous form lost its chemotherapy indication in 2010 because of heart rhythm effects.","summary":"Dolasetron, approved by the FDA in September 1997, joined ondansetron and granisetron as a first-generation 5-HT3 antagonist for prevention of nausea and vomiting from moderately emetogenic chemotherapy and after surgery. It is a prodrug converted to hydrodolasetron. In 2010 the FDA contraindicated the intravenous form for chemotherapy-induced nausea because of dose-dependent QT prolongation and arrhythmias, leaving the tablets. Guidelines treat the first-generation agents as interchangeable for acute emesis, with palonosetron preferred for delayed emesis and NK1 antagonists and olanzapine added for highly emetogenic regimens.","status":"established","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Dolasetron","links":[{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=dolasetron"},{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Dolasetron"},{"label":"ChEMBL CHEMBL1200880","url":"https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200880"}],"tags":["gap-fill","chembl-universe"],"related":[],"cancers":[],"sections":[],"technologies":[],"targets":["htr3a"],"drugs":["ondansetron","granisetron","palonosetron"],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"notes":[],"brand":"Anzemet","modality":"Oral 5-HT3 receptor antagonist antiemetic","mechanism":"Blocks 5-HT3 serotonin receptors on vagal nerve endings in the gut and in the brainstem, cutting the signal that chemotherapy-released serotonin sends to the vomiting centre.","approvals":[{"region":"US","year":1997,"indication":"Prevention of nausea and vomiting from moderately emetogenic chemotherapy (oral); intravenous chemotherapy indication removed in 2010"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/dolasetron/","neighbours":{"target":[{"id":"htr3a","kind":"target","name":"5-HT3 receptor (HTR3A)","route":"/targets/htr3a/"}],"drug":[{"id":"granisetron","kind":"drug","name":"Granisetron","route":"/drugs/granisetron/"},{"id":"ondansetron","kind":"drug","name":"Ondansetron","route":"/drugs/ondansetron/"},{"id":"palonosetron","kind":"drug","name":"Palonosetron","route":"/drugs/palonosetron/"}]}}